Macrocyclic peptides as drug candidates: recent progress and remaining challenges
AA Vinogradov, Y Yin, H Suga - Journal of the American Chemical …, 2019 - ACS Publications
Peptides as a therapeutic modality attract much attention due to their synthetic accessibility,
high degree of specific binding, and the ability to target protein surfaces traditionally …
high degree of specific binding, and the ability to target protein surfaces traditionally …
Supramolecular luminescent sensors
TL Mako, JM Racicot, M Levine - Chemical reviews, 2018 - ACS Publications
There is great need for stand-alone luminescence-based chemosensors that exemplify
selectivity, sensitivity, and applicability and that overcome the challenges that arise from …
selectivity, sensitivity, and applicability and that overcome the challenges that arise from …
Orally absorbed cyclic peptides
DS Nielsen, NE Shepherd, W Xu, AJ Lucke… - Chemical …, 2017 - ACS Publications
Peptides and proteins are not orally bioavailable in mammals, although a few peptides are
intestinally absorbed in small amounts. Polypeptides are generally too large and polar to …
intestinally absorbed in small amounts. Polypeptides are generally too large and polar to …
[HTML][HTML] Systemic delivery of peptides by the oral route: Formulation and medicinal chemistry approaches
In its 33 years, ADDR has published regularly on the po5tential of oral delivery of biologics
especially peptides and proteins. In the intervening period, analysis of the preclinical and …
especially peptides and proteins. In the intervening period, analysis of the preclinical and …
Cyclic peptides as drugs for intracellular targets: the next frontier in peptide therapeutic development
LK Buckton, MN Rahimi… - Chemistry–A European …, 2021 - Wiley Online Library
Developing macrocyclic peptides that can reach intracellular targets is a significant
challenge. This review discusses the most recent strategies used to develop cell permeable …
challenge. This review discusses the most recent strategies used to develop cell permeable …
Strategies for fine-tuning the conformations of cyclic peptides
Cyclic peptides are promising scaffolds for drug development, attributable in part to their
increased conformational order compared to linear peptides. However, when optimizing the …
increased conformational order compared to linear peptides. However, when optimizing the …
Lipophilic permeability efficiency reconciles the opposing roles of lipophilicity in membrane permeability and aqueous solubility
MR Naylor, AM Ly, MJ Handford… - Journal of medicinal …, 2018 - ACS Publications
As drug discovery moves increasingly toward previously “undruggable” targets such as
protein–protein interactions, lead compounds are becoming larger and more lipophilic …
protein–protein interactions, lead compounds are becoming larger and more lipophilic …
Improving drug design: an update on recent applications of efficiency metrics, strategies for replacing problematic elements, and compounds in nontraditional drug …
NA Meanwell - Chemical Research in Toxicology, 2016 - ACS Publications
Drug discovery and development is a complex and lengthy enterprise that suffers from high
rates of candidate attrition at all stages of the process. The physical, biological, and …
rates of candidate attrition at all stages of the process. The physical, biological, and …
Cyclic and macrocyclic peptides as chemical tools to recognise protein surfaces and probe protein–protein interactions
TAF Cardote, A Ciulli - ChemMedChem, 2016 - Wiley Online Library
Targeting protein surfaces and protein–protein interactions (PPIs) with small molecules is a
frontier goal of chemical biology and provides attractive therapeutic opportunities in drug …
frontier goal of chemical biology and provides attractive therapeutic opportunities in drug …
Conformational Control of Macrocycles by Remote Structural Modification: Focus Review
SD Appavoo, S Huh, DB Diaz, AK Yudin - Chemical reviews, 2019 - ACS Publications
The conformational analysis of macrocycles is a complex and challenging problem. There
are many factors that contribute to this complexity. These include a large number of degrees …
are many factors that contribute to this complexity. These include a large number of degrees …